EP3366676A4 - Crystalline forms of bedaquiline fumarate and preparation methods therefor - Google Patents
Crystalline forms of bedaquiline fumarate and preparation methods therefor Download PDFInfo
- Publication number
- EP3366676A4 EP3366676A4 EP15906444.3A EP15906444A EP3366676A4 EP 3366676 A4 EP3366676 A4 EP 3366676A4 EP 15906444 A EP15906444 A EP 15906444A EP 3366676 A4 EP3366676 A4 EP 3366676A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- preparation methods
- crystalline forms
- methods therefor
- bedaquiline fumarate
- bedaquiline
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 229960001137 bedaquiline fumarate Drugs 0.000 title 1
- ZLVSPMRFRHMMOY-WWCCMVHESA-N bedaquiline fumarate Chemical compound OC(=O)\C=C\C(O)=O.C1([C@H](C2=CC3=CC(Br)=CC=C3N=C2OC)[C@@](O)(CCN(C)C)C=2C3=CC=CC=C3C=CC=2)=CC=CC=C1 ZLVSPMRFRHMMOY-WWCCMVHESA-N 0.000 title 1
- 238000002360 preparation method Methods 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
- C07D215/22—Oxygen atoms attached in position 2 or 4
- C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
- B01D—SEPARATION
- B01D9/00—Crystallisation
- B01D9/0063—Control or regulation
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A61P31/06—Antibacterial agents for tuberculosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pulmonology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- General Chemical & Material Sciences (AREA)
- Crystallography & Structural Chemistry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Quinoline Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/CN2015/092343 WO2017066926A1 (en) | 2015-10-20 | 2015-10-20 | Crystalline forms of bedaquiline fumarate and preparation methods therefor |
Publications (3)
Publication Number | Publication Date |
---|---|
EP3366676A1 EP3366676A1 (en) | 2018-08-29 |
EP3366676A4 true EP3366676A4 (en) | 2019-06-12 |
EP3366676B1 EP3366676B1 (en) | 2021-05-26 |
Family
ID=58556625
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP15906444.3A Active EP3366676B1 (en) | 2015-10-20 | 2015-10-20 | Crystalline forms of bedaquiline fumarate and preparation methods therefor |
Country Status (6)
Country | Link |
---|---|
US (1) | US10196360B2 (en) |
EP (1) | EP3366676B1 (en) |
KR (1) | KR102106318B1 (en) |
CN (1) | CN108349898B (en) |
RU (1) | RU2018111482A (en) |
WO (1) | WO2017066926A1 (en) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PL3651736T3 (en) * | 2017-07-14 | 2021-12-20 | Janssen Pharmaceutica Nv | Long-acting formulations |
KR102303635B1 (en) * | 2020-07-01 | 2021-09-17 | 동아에스티 주식회사 | PROCESS FOR PREPARING (1R,2S)-1-(6-bromo-2-methoxyquinolin-3-yl)-4-dimethylamino-2-(1-naphthyl)-1-phenyl-butan-2-ol AND PHARMACEUTICALLY ACCEPTABLE SALT |
CN111606850B (en) * | 2020-07-07 | 2023-07-25 | 安徽贝克生物制药有限公司 | Preparation method of bedaquiline and intermediate thereof |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2008068231A1 (en) * | 2006-12-05 | 2008-06-12 | Janssen Pharmaceutica N.V. | Fumarate salt of (alpha s, beta r)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1325475C (en) * | 2002-07-25 | 2007-07-11 | 詹森药业有限公司 | Quinoline derivatives and their use as mycobacterial inhibitors |
CN1976704B (en) * | 2004-05-28 | 2012-12-05 | 詹森药业有限公司 | Use of substituted quinoline derivatives for the treatment of drug resistant mycobacterial diseases |
CZ2014708A3 (en) * | 2014-10-16 | 2016-04-27 | Zentiva, K.S. | Bedaqujiline salts |
CN106279017A (en) * | 2015-05-21 | 2017-01-04 | 重庆圣华曦药业股份有限公司 | Bedaquinoline crystal form, composition and preparation method thereof |
CN106316943A (en) * | 2016-07-27 | 2017-01-11 | 重庆华邦制药有限公司 | Refining method of bedaquiline fumarate crystal form compound |
-
2015
- 2015-10-20 KR KR1020187013042A patent/KR102106318B1/en active IP Right Grant
- 2015-10-20 EP EP15906444.3A patent/EP3366676B1/en active Active
- 2015-10-20 US US15/760,090 patent/US10196360B2/en active Active
- 2015-10-20 CN CN201580083040.XA patent/CN108349898B/en active Active
- 2015-10-20 WO PCT/CN2015/092343 patent/WO2017066926A1/en active Application Filing
- 2015-10-20 RU RU2018111482A patent/RU2018111482A/en unknown
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2008068231A1 (en) * | 2006-12-05 | 2008-06-12 | Janssen Pharmaceutica N.V. | Fumarate salt of (alpha s, beta r)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol |
Non-Patent Citations (2)
Title |
---|
CAIRA M R ED - MONTCHAMP JEAN-LUC: "CRYSTALLINE POLYMORPHISM OF ORGANIC COMPOUNDS", TOPICS IN CURRENT CHEMISTRY; [TOPICS IN CURRENT CHEMISTRY], SPRINGER, BERLIN, DE, vol. 198, 1 January 1998 (1998-01-01), pages 163 - 208, XP001156954, ISSN: 0340-1022, DOI: 10.1007/3-540-69178-2_5 * |
See also references of WO2017066926A1 * |
Also Published As
Publication number | Publication date |
---|---|
WO2017066926A1 (en) | 2017-04-27 |
KR102106318B1 (en) | 2020-05-06 |
EP3366676A1 (en) | 2018-08-29 |
CN108349898A (en) | 2018-07-31 |
CN108349898B (en) | 2021-03-23 |
US10196360B2 (en) | 2019-02-05 |
RU2018111482A (en) | 2019-11-21 |
KR20180059941A (en) | 2018-06-05 |
EP3366676B1 (en) | 2021-05-26 |
RU2018111482A3 (en) | 2019-11-21 |
US20180265473A1 (en) | 2018-09-20 |
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